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Pinometostat (EPZ5676) DOT1L inhibitor

Cat.No.S7062

Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.
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Quality Control

Batch: Purity: 99.99%
99.99
Q&A of Pinometostat (EPZ5676): Insights Rooted in Extensive Publications, Every Answer Cited
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Solubility in DMSO or Water

In vitro
Batch:

DMSO : 100 mg/mL (177.71 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass Concentration Volume Molecular Weight
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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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g
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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Working Concentrations for Cell Culture Treatment

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Mechanism of Action

Information Pinometostat (EPZ5676) is a selective DOT1L inhibitor. It affects IFN-Stat1, STING, and WNT signaling pathways by reducing H3K79 methylation and downregulating target genes, effectively inhibiting cancer cell proliferation, stemness, and promoting apoptosis.
Primary Applications and Mechanism of Action

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Chemical Information, Storage & Stability

Molecular Weight 562.71 Formula

C30H42N8O3

Storage (From the date of receipt)
CAS No. 1380288-87-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(C)N(CC1C(C(C(O1)N2C=NC3=C(N=CN=C32)N)O)O)C4CC(C4)CCC5=NC6=C(N5)C=C(C=C6)C(C)(C)C

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Handling Instructions

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Frequently Asked Questions

Question 1:
Is the vehicle 30% PEG400/0.5% Tween80/5% propylene glycol recommended for in vivo use?

Answer:
S7062 in 30% PEG400/0.5% Tween80/5% propylene glycol at 30 mg/ml is a suspension. For injection, 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml is suitable.